2-Hydroxymethyl-4-[5-(4-methoxyphenyl)-3-trifluoromethyl-1 H-1-pyrazolyl]-1-benzenesulfonamide (DRF-4367): an orally active COX-2 inhibitor identified through …

…, R Mullangi, R Bhamidipati, R Ramanujam…

Index: Singh, Sunil Kumar; Vobbalareddy, Saibaba; Kalleda, Srinivasa Rao; Rajjak, Shaikh Abdul; Casturi, Seshagiri Rao; Datla, Srinivasa Raju; Mamidi, Rao N.V.S.; Mullangi, Ramesh; Bhamidipati, Ravikanth; Ramanujam, Rajagopalan; Akella, Venkateswarlu; Yeleswarapu, Koteswar Rao Organic and Biomolecular Chemistry, 2004 , vol. 2, # 17 p. 2442 - 2450

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Citation Number: 15

Abstract

Analogs of 1, 5-diarylpyrazoles with a novel pharmacophore at N1 were designed, synthesized and evaluated for the in-vitro cyclooxygenase (COX-1/COX-2) inhibitory activity. The variations at/around position-4 of the C-5 phenyl ring in conjunction with a CF3 and CHF2 groups at C-3 exhibited a high degree of potency and selectivity index (SI) for COX-2 inhibition. The in-vivo evaluation of these potent compounds with a few earlier ones ...